打敗癌症最好的方法是「早期診斷、早期治療」。因為正子放射斷層掃描(PET)和單光子放射電腦斷層掃描(SPECT)的發明與使用，使用具有標靶癌症功能的放射性分子，作非侵入式顯影診斷癌症得以施行。為了有效地發展具有標靶癌症功能的放射性分子，本實驗室因而使用了創新的方法：快速的平行合成液相分子庫(solution phase derived synthetic libraries)，並以細胞為平台(cell-based platforms)，作其原位的生物活性篩選(in-situ screening)。我們有興趣的核心結構可分為兩種： 一種是和天然物類似(natural product-like)，另一種是和目前現有的藥物類似(drug-like)，有包括核苷(nucleoside)、醣(glycoside)、醣化神經醯脂質(glycosphingolipid)、神經醯胺(ceramide)、植物鞘胺醇(phytosphingosine)、利尿酸醯胺(ethacrynic amide)、芬布芬醯胺(fenbufen amide)、榖胱甘肽(glutathione)、環形胜肽(cyclic peptide)…諸如此類。為了配合正子放射斷層掃描(PET)，考慮適合的半衰期核種，半衰期約為兩個小時的氟十八，是好的放射化學標誌選擇；若是配合單光子放射電腦斷層掃描(SPECT)，亦考慮適合的半衰期核種，半衰期約為六個小時的鎝99m和十三個小時的碘一二三，是兩種適當的放射化學標誌選擇。這些被合成出的具有生物活性之放射性標誌分子(radiolabeled bioactive molecules)，除了可能進一步地漸漸發展成臨床用藥之外，尚可以很容易的作為藥物代謝(metabolism)和藥物動力學(pharmacokinetics & pharmacodynamics)之研究探針，又因為放射線的高能量和探針分子的低濃度，其優點是高度的敏感性和低度的化學毒性。時至目前，我們實驗室已經有一些放射性標誌的生物活性分子(radiolabeled bioactive molecules)已合成出，並已進入前臨床研究(preclinical trials)的階段，希望在不久的未來，會有進入至臨床研究(clinical trials)的放射性標誌分子。

Early diagnosis of cancer is the best way to beat cancer. Because of PET (positron emission tomography) and SPECT (single-photon emission computed tomography), cancer-targeted radiolabeled molecules can be monitored by non-invasive imaging for diagnosis. In order to develop cancer-targeted radiolabeled molecules efficiently, rapid parallel synthesis of solution-phase derived libraries followed by their in situ cell-based screening is an innovative approach. The core structures are natural product-like and drug-like molecules, including nucleoside, glycoside, glycosphingolipid, ceramide, phytosphingosine, ethacrynic amide, fenbufen amide, glutathione, cyclic peptide and so on. The proper radionuclides are fluorine-18, iodine-123, Tc-99m and …etc. In addition to diagnosis, radiolabeled bioactive molecules can be easily used for studies of their metabolites, pharmacokinetics, pharmacodynamics due to high sensitivity and low toxicity. Some of radiolabeled bioactive molecules have been studied in preclinical phase and their clinical trials might be performed in the future.